Click reaction based synthesis, antimicrobial, and cytotoxic activities of new 1,2,3-triazoles.

Autor: El Sayed Aly MR; Chemistry Department, Faculty of Science, Taif University, Hawyah-Taif, Saudi Arabia; Chemistry Department, Faculty of Applied Science, Port Said University, 42522 Port Said, Egypt. Electronic address: mrea34@hotmail.com., Saad HA; Chemistry Department, Faculty of Science, Taif University, Hawyah-Taif, Saudi Arabia; Chemistry Department, Faculty of Science, Zagazig University, Zagazig 44511, Egypt., Mohamed MA; Chemistry Department, Faculty of Science, Taif University, Hawyah-Taif, Saudi Arabia; Chemistry Department, Faculty of Science, Cairo University, Cairo 12613, Egypt.
Jazyk: angličtina
Zdroj: Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Jul 15; Vol. 25 (14), pp. 2824-30. Date of Electronic Publication: 2015 May 06.
DOI: 10.1016/j.bmcl.2015.04.096
Abstrakt: Three-motif pharmacophoric models 20a-e and 21-25 were prepared in good yields by CuAAC of two azido substrates 2 and 11 with seven terminal acetylenic derivatives including chalcones 17a-e, theophylline 18 and cholesterol 19. The structure of these compounds was elucidated by NMR, MS, IR spectroscopy and micro analyses. This series was screened as antimicrobial and cytotoxic agents in vitro. Most derivatives showed appreciable antibacterial activity, but they displayed weak cytotoxic, and antifungal activities. Notably, conjugate 25 (cream of the crop) was found to be more active than Ampicillin against Escherichia coli and Staphylococcus aureus and showed appreciable antifungal and cytotoxic activities as well.
(Copyright © 2015 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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